黄体酮在大鼠脂肪前体细胞中与糖皮质激素受体结合并介导抗糖皮质激素作用

Xuefan Xu , Johan Hoebeke , Per Björntorp
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引用次数: 57

摘要

研究了大鼠脂肪前体细胞细胞质中黄体酮与糖皮质激素的结合。以[3H]R5020为放射配体,雌性大鼠脂肪前体细胞细胞质中存在高亲和力和有限容量的黄体酮结合位点,而雄性大鼠脂肪前体细胞细胞质中没有。以[3H]地塞米松和[3H]曲安奈德为放射配体,在雄性和雌性大鼠这些细胞的细胞质中均存在高亲和力和有限容量的糖皮质激素结合位点。解离常数在生理浓度范围内。竞争结合的研究表明,黄体酮可以在糖皮质激素结合位点与糖皮质激素竞争。在无血清培养基中,糖皮质激素对细胞分化的影响由甘油磷酸脱氢酶(GPDH)监测,可被黄体酮有效抵消,而黄体酮本身没有作用。结果表明,黄体酮受体仅存在于雌性大鼠脂肪前体细胞中,糖皮质激素受体存在于两性大鼠脂肪前体细胞中。糖皮质激素对这些细胞分化的影响是由糖皮质激素受体介导的。黄体酮结合糖皮质激素受体,拮抗糖皮质激素对这些细胞分化的影响。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Progestin binds to the glucocorticoid receptor and mediates antiglucocorticoid effect in rat adipose precursor cells

The binding of progestin and glucocorticoid hormones was examined in the cytosol of rat adipose precursor cells. Progestin binding sites of high affinity and limited capacity were present in the cytosol of adipose precursor cells from female rats, but not from male rats, by using [3H]R5020 as radioligand. Glucocorticoid binding sites of high affinity and limited capacity were present in the cytosol of these cells from both male and female rats by using [3H]dexamethasone and [3H]triamcinolone acetonide as radioligands. The dissociation constants were in the physiological concentration range. Studies of competitive binding showed that progestin could compete with glucocorticoids at glucocorticoid binding sites. In a serum free medium glucocorticoid effect on cellular differentiation, monitored by glycerophosphate dehydrogenase (GPDH), was effectively counteracted by progesterone which by itself had no effect.

These results demonstrate that progestin receptor exists only in rat adipose precursor cells from female rats, while glucocorticoid receptor exists in rat adipose precursor cells of both sexes. Glucocorticoid effects on cellular differentiation in these cells are mediated by the glucocorticoid receptor. Progestin binds to the glucocorticoid receptor and antagonizes glucocorticoid effect on cellular differentiation in these cells.

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